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A procedure has been developed for the synthesis of functional isoxazole and isothiazole derivatives by reduction of (5-aryl-1,2-oxazol-3-yl)methoxybenzaldehydes to (5-aryl-1,2-oxazol-3-yl)methoxyaryl-methanols and subsequent acylation of the latter with isoxazole- and isothiazolecarbonyl chlorides.

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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

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A series of 1,1-dioxothieno[2,3-d]isothiazole (thienosultam) derivatives were designed and synthesized as novel ADAMTS-5 inhibitors for an investigation into a side chain of thienosultam for the S1′ pocket. The resulting compounds (19 and 24) show high ADAMTS-5 inhibition and other MMP selectivity, and these compounds show good oral bioavailability. (C) 2013 Elsevier Ltd. All rights reserved.

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In this study, we have determined and compared the pharmacological profiles of ibotenic acid and its isothiazole analogue thioibotenic acid at native rat ionotropic glutamate (iGlu) receptors and at recombinant rat metabotropic glutamate (mGlu) receptors expressed in mammalian cell lines. Thioibotenic acid has a distinct pharmacological profile at group III mGlu receptors compared with the closely structurally related ibotenic acid; the former is a potent (low mum) agonist, whereas the latter is inactive. By comparing the conformational energy profiles of ibotenic and thioibotenic acid with the conformations preferred by the ligands upon docking to mGlu(1) and models of the other mGlu subtypes, we propose that unlike other subtypes, group III mGlu receptor binding sites require a ligand conformation at an energy level which is prohibitively expensive for ibotenic acid, but not for thioibotenic acid. These studies demonstrate how subtle differences in chemical structures can result in profound differences in pharmacological activity. (C) 2004 Elsevier B.V. All rights reserved.

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New Advances in Chemical Research in 2021, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 3466-32-8, Name is 1-Bromo-4-(methylsulfonyl)benzene, molecular formula is C7H7BrO2S, belongs to isothiazole compound. In a document, author is Hermit, MB, introduce the new discover, Formula: https://www.ambeed.com/products/3466-32-8.html.

In this study, we have determined and compared the pharmacological profiles of ibotenic acid and its isothiazole analogue thioibotenic acid at native rat ionotropic glutamate (iGlu) receptors and at recombinant rat metabotropic glutamate (mGlu) receptors expressed in mammalian cell lines. Thioibotenic acid has a distinct pharmacological profile at group III mGlu receptors compared with the closely structurally related ibotenic acid; the former is a potent (low mum) agonist, whereas the latter is inactive. By comparing the conformational energy profiles of ibotenic and thioibotenic acid with the conformations preferred by the ligands upon docking to mGlu(1) and models of the other mGlu subtypes, we propose that unlike other subtypes, group III mGlu receptor binding sites require a ligand conformation at an energy level which is prohibitively expensive for ibotenic acid, but not for thioibotenic acid. These studies demonstrate how subtle differences in chemical structures can result in profound differences in pharmacological activity. (C) 2004 Elsevier B.V. All rights reserved.

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New Advances in Chemical Research in 2021. COA of Formula: https://www.ambeed.com/products/3466-32-8.html, You could be based in a university, combining chemical research with teaching; in a pharmaceutical company, working on developing and trialing new drugs; helping to ensure national healthcare provision keeps pace with new discoveries. 3466-32-8, Name is 1-Bromo-4-(methylsulfonyl)benzene, SMILES is O=S(C1=CC=C(Br)C=C1)(C)=O, belongs to isothiazole compound. In a article, author is Ioannidou, Heraklidia A., introduce new discover of the category.

The conversion of isothiazoles into pyrazoles on treatment with hydrazine is investigated. The influence of various C-3, C-4 and C-5 isothiazole substituents and some limitations of this ring transformation are examined. When the isothiazole C-3 substituent is a good nucleofuge, 3-aminopyrazoles are obtained. However, when the 3-substituent is not a leaving group it is retained in the pyrazole product. Treatment of 4-bromo-3-chloro-5-phenylisothiazoie 56 or 3-chloro-4,5-diphenylisothiazole 57 with anhydrous hydrazine at ca. 200 degrees C for a few minutes gives the corresponding 3-hydrazinoisothiazoles 61 and 64 respectively in high yields; the stability of these new hydrazines is investigated. 5,5′-Diphenyl-3,3′-biisothiazole-4,4′-dicarbonitrile 78 reacts with hydrazine to give 5,5′-diphenyl-3,3′-bi(1H-pyi-azole)-4,4′-dicarbonitrile 79. Methylhydrazine reacts with 3-chloro-5-phenytisothiazole-4-carbonitrile 1 to give 3-(1-methylhydrazino)-5-phenylisothiazole-4-carbontrile 83 and 3-amino-lmethyl-5-phenylpyrazole-4-carbonitrile 84. All products are fully characterised and rational mechanisms for the isothiazole into pyrazole transformation are proposed. (C) 2009 Elsevier Ltd. All rights reserved.

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New discoveries in chemical research and development in 2021, Chemistry involves the study of all things chemical – chemical processes, how they change and how they react in certain situations. 3466-32-8, Name is 1-Bromo-4-(methylsulfonyl)benzene, SMILES is O=S(C1=CC=C(Br)C=C1)(C)=O, in an article , author is OHKATA, K, once mentioned of 3466-32-8, Electric Literature of 3466-32-8.

In the presence of 1,4-diazabicyclo[2.2.2]octane, 5-amino-3-methylisothiazole (4a) in acetonitrile condensed with N-methyl-p-chlorobenzimidoyl chloride (5a) to afford two kinds of compounds along with several minor products. One of the two was 1 : 1 condensed product (6a) and the other was 2 : 1 condensed product (7a). The latter compound was obtained in higher yield when an excess 4a was treated with 5a. On the other hand, in the absence of the additional base, 2 : 3 condensed compound (8a) was isolated as a major product besides 6a and 7a. 8a was obtained by treatment of 7a with 2 equiv. of imidoyl chloride in 21% yield. Reaction of 5-amino-3-phenylisothiazole (4b) with imidoyl chloride (5a,b) furnished the analogous products. On the other hand, condensation of 5-amino-3-phenylisoxazole (4c) with 5a furnished the oxygen analogue (6d) corresponding to 6b as a sole isolated product. The formation of 7 is explained by ring-transformation from isothiazole into thiadiazole via hypervalent 10-S-3 type sulfurane (B). According to a variety of investigations of heterocycles containing sulfur atom, it has been suggested that 10-S-3 type sulfurane is an important intermediate in several reactions.1,2. In a previous paper, we reported that a ring transformed thiadiazole derivative (1) instead of the expected isothiazole derivative (2) was isolated as a sole product in the reaction of 5-amino-3-methylisothiazole with arylnitrile.3a The fact was explained by invoking 10-S-3 sulfurane (A) as a intermediate. In connection with this finding, we describe in this paper results of the reaction of 5-aminoisoazole derivatives (4a-c) with imidoyl chloride (5a,b) under several conditions.

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A series of 1,1-dioxothieno[2,3-d]isothiazole (thienosultam) derivatives were designed and synthesized as novel ADAMTS-5 inhibitors for an investigation into a side chain of thienosultam for the S1′ pocket. The resulting compounds (19 and 24) show high ADAMTS-5 inhibition and other MMP selectivity, and these compounds show good oral bioavailability. (C) 2013 Elsevier Ltd. All rights reserved.

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The developments in the synthesis of the five-membered heterocycles with one pnictogen (As, Sb, Bi) heteroatom have in the last 15 years or so been practically focused only on three types of compounds: saturated or unsaturated pnictogenoles, monofused pnictogenoles, and diffused pnictogenoles, where the fused ring is benzene, thiophene, isothiazole, benzothiophene, or benzofuran. Trendy is preparation and tuning of the optoelectronic properties of the target compounds, their complexes or polymers, respectively. Almost all syntheses of nearly all systems are based on transmetallation of lithium (for 1,3-diene known as Ashe’s method), potassium, Grignard, copper, titanium, or zirconium species (Fagan-Nugent zirconium metallacycle-transfer method), regardless of whether the system is saturated (as is the case for the majority of compounds) or unsaturated.

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A procedure has been developed for the synthesis of functional isoxazole and isothiazole derivatives by reduction of (5-aryl-1,2-oxazol-3-yl)methoxybenzaldehydes to (5-aryl-1,2-oxazol-3-yl)methoxyaryl-methanols and subsequent acylation of the latter with isoxazole- and isothiazolecarbonyl chlorides.

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Chemical Research Letters, April 2021. Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. 3466-32-8, Name is 1-Bromo-4-(methylsulfonyl)benzene, molecular formula is C7H7BrO2S, Recommanded Product: 3466-32-8, belongs to isothiazole compound, is a common compound. In a patnet, author is Schulze, B, once mentioned the new application about 3466-32-8.

This review gives a report of the last ten years on the new synthetic methods, reactions and biological applications of isothiazole 1,1-dioxide derivatives. The formation of monocyclic and heterocyclic annelated isothiazole 1,1-dioxides by oxidation of isothiazoles, cyclocondensation of sulfonamides and cycloaddition of isothiazol-3 (2H)-one 1,1-dioxides are discussed in more detail. Furthermore, the preparation of pharmacologically important N-substituted saccharines is reported. New saccharine-derived chiral N-enoyl- and N-acyl-2,3-dihydro-1,2-benzisothiazole 1,1-dioxides serve as advantageous stereoface-directing dienophile and dipolarophile auxiliaries in Diels-Alder-reactions and 1,3-dipolar cycloadditions. Asymmetric alkylations, acylations and aldolizations are also described.

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